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    Indoloylguanidine derivatives
    1.
    发明授权
    Indoloylguanidine derivatives 失效

    公开(公告)号：US06248772B1

    公开(公告)日：2001-06-19

    申请号：US09604826

    申请日：2000-06-27

    申请人： Masahumi Kitano ,  Kazuhiro Nakano ,  Hideki Yagi ,  Naohito Ohashi ,  Atsuyuki Kojima ,  Tsuyoshi Noguchi ,  Akira Miyagishi

    发明人： Masahumi Kitano ,  Kazuhiro Nakano ,  Hideki Yagi ,  Naohito Ohashi ,  Atsuyuki Kojima ,  Tsuyoshi Noguchi ,  Akira Miyagishi

    IPC分类号： A61K31404

    CPC分类号： C07D209/08 ,  C07D209/42

    摘要： Novel indoloylguanidine derivatives shown by formula (1), wherein R1 represents one or more, the same or different substituent(s) which is selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen atom, nitro group, an acyl group, carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group shown by formula: —OR3, —NR6R7, —SO2NR6R7 or —S(O)nR40; and R2 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, hydroxy group, an alkoxy group or a group shown by formula: —CH2R20; and which inhibit the Na+/H+ exchanger activity and are useful for the treatment and prevention of a disease caused by increased Na+/H+ exchanger activity, such as hypertension, arrhythmia, angina pectoris, cardiac hypertrophy, diabetes, disorders associated with ischemia or ischemic reperfusion, cerebro-ischemic disorders; or diseases caused by excessive cell proliferation.

    Indoloylguanidine derivatives
    2.
    发明授权
    Indoloylguanidine derivatives 失效
    吲哚酰胍衍生物

    公开(公告)号：US06169107A

    公开(公告)日：2001-01-02

    申请号：US08544292

    申请日：1995-10-17

    申请人： Masahumi Kitano ,  Kazuhiro Nakano ,  Hideki Yagi ,  Naohito Ohashi ,  Atsuyuki Kojima ,  Tsuyoshi Noguchi ,  Akira Miyagishi

    发明人： Masahumi Kitano ,  Kazuhiro Nakano ,  Hideki Yagi ,  Naohito Ohashi ,  Atsuyuki Kojima ,  Tsuyoshi Noguchi ,  Akira Miyagishi

    IPC分类号： A61K31404

    CPC分类号： C07D209/08 ,  C07D209/42

    摘要： Novel indoloylguanidine derivatives shown by formula (1), wherein R1 represents one or more, the same or different substituent(s) which is selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen atom, nitro group, an acyl group, carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group shown by formula: —OR3, —NR6R7, —SO2NR6R7 or —S(O)nR40; and R2 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, hydroxy group, an alkoxy group or a group shown by formula: —CH2R20; and which inhibit the Na+/H+ exchanger activity and are useful for the treatment and prevention of a disease caused by increased Na+/H+ exchanger activity, such as hypertension, arrhythmia, angina pectoris, cardiac hypertrophy, diabetes, disorders associated with ischemia or ischemic reperfusion, cerebro-ischemic disorders; or diseases caused by excessive cell proliferation.

    摘要翻译： 式（1）所示的新型吲哚酰基胍衍生物，其中R1表示一个或多个选自氢原子，烷基，取代的烷基，烯基， 炔基，环烷基，卤素原子，硝基，酰基，羧基，烷氧基羰基，芳香族基团和由下式表示的基团：-OR3，-NR6R7，-SO2NR6R7或-S（O ）nR40; R2表示氢原子，烷基，取代的烷基，环烷基，羟基，烷氧基或由式-CH2R20表示的基团; 并且其抑制Na + / H +交换活性，并且可用于治疗和预防由升高的Na + / H +交换活性引起的疾病，例如高血压，心律失常，心绞痛，心脏肥大，糖尿病，与缺血或缺血再灌注相关的疾病 ，脑缺血障碍; 或由过度细胞增殖引起的疾病。

    Substituted guanidine derivatives and process for producing the same
    4.
    发明授权
    Substituted guanidine derivatives and process for producing the same 失效
    取代的胍衍生物及其制备方法

    公开(公告)号：US06369110B1

    公开(公告)日：2002-04-09

    申请号：US09701269

    申请日：2000-11-27

    申请人： Masahumi Kitano ,  Naohito Ohashi

    发明人： Masahumi Kitano ,  Naohito Ohashi

    IPC分类号： C07C27902

    CPC分类号： C07D223/16 ,  C07C279/22 ,  C07C317/44 ,  C07C323/62 ,  C07C2602/10 ,  C07C2602/12 ,  C07D215/54 ,  C07D225/06

    摘要： A compound represented by the general formula (1): wherein each of R1, R2, R3, R4 and R5 is a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, an aromatic group, an acyl group or the like; each of Y1, Y2, Y3 and Y4 is a single bond, —CH2—, —O—, —CO— or the like, provided that at least two of Y1 through Y4 are independently a group other than a single bond; and Z may be absent, or one or more Zs may be present and are independently an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, a halogen atom, a carboxyl group, an alkoxycarbonyl group, an aromatic group, an acyl group or the like, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton exchange transport system.

    摘要翻译： 由通式（1）表示的化合物：其中R 1，R 2，R 3，R 4和R 5各自为氢原子，烷基，取代的烷基，烯基，炔基，环烷基， 环烯基，饱和杂环基，芳基，酰基等; Y 1，Y 2，Y 3和Y 4中的每一个为单键，-CH 2 - ， - O - ， - CO-等，条件是Y 1至Y 4中的至少两个独立地为除单键以外的基团。 Z可以不存在，也可以是一个以上的Z，可以独立地为烷基，取代的烷基，烯基，炔基，环烷基，环烯基，饱和杂环基，卤素原子， 羧基，烷氧基羰基，芳香族基，酰基等可用作由加速钠/质子交换系统引起的疾病的治疗或预防剂。

    Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof
    5.
    发明授权
    Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof 失效
    取代的胍衍生物，其制备方法及其药物用途

    公开(公告)号：US06271251B1

    公开(公告)日：2001-08-07

    申请号：US09342101

    申请日：1999-06-29

    申请人： Masahumi Kitano ,  Naohito Ohashi

    发明人： Masahumi Kitano ,  Naohito Ohashi

    IPC分类号： A61K3140

    CPC分类号： C07D471/06 ,  C07D487/06

    摘要： A substituted guanidine derivative represented by the general formula: or a pharmaceutically acceptable acid addition salt thereof, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton (Na+/H+) exchange transport system, for example, hyperpiesia, arrhythmia, angina pectoris, hypercardia, diabetes, organopathies due to ischemia or ischemia re-perfusion, troubles due to cerebral ischemia, diseases caused by cell over-proliferations, and diseases caused by trouble with endothelial cells.

    摘要翻译： 由通式表示的取代的胍衍生物或其药学上可接受的酸加成盐可用作由加速钠/质子（Na + / H +）交换转运系统引起的疾病的治疗或预防剂，例如， 高血压，心律失常，心绞痛，高血压，糖尿病，由于局部缺血或缺血再灌注引起的有机病变，由于脑缺血引起的麻烦，由细胞过度增殖引起的疾病以及由内皮细胞引起的疾病引起的疾病。

    Substituted guanidine derivatives
    6.
    发明授权
    Substituted guanidine derivatives 失效
    取代的胍衍生物

    公开(公告)号：US06734205B2

    公开(公告)日：2004-05-11

    申请号：US10168112

    申请日：2002-06-17

    申请人： Masahumi Kitano ,  Masatoshi Yuri ,  Naohito Ohashi

    发明人： Masahumi Kitano ,  Masatoshi Yuri ,  Naohito Ohashi

    IPC分类号： A61K31404

    CPC分类号： C07F9/5728 ,  C07D209/42 ,  C07H17/02

    摘要： A compound represented by the following formula: wherein R is a substituted or unsubstituted benzene ring, a fused polycyclic hydrocarbon ring which is substituted or unsubstituted, a monocyclic heterocyclic ring which is substituted or unsubstituted, a polycyclic heterocyclic ring which is substituted or unsubstituted, A and E are independently a single bond, a lower alkylene group or the like, G is a single bond, an oxygen atom or the like, and Y is a —SO3H group or the like, a prodrug of said compound, or a pharmaceutically acceptable salt of said compound or prodrug is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton exchange transport system.

    摘要翻译： 由下式表示的化合物：其中R是取代或未取代的苯环，被取代或未取代的稠合多环烃环，被取代或未取代的单环杂环，被取代或未取代的多环杂环，A E独立地为单键，低级亚烷基等，G为单键，氧原子等，Y为-SO 3 H基等，所述化合物的前药或药学上可接受的 所述化合物或前药的盐可用作由加速钠/质子交换转运系统引起的疾病的治疗或预防剂。

    Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof
    7.
    发明授权
    Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof 失效
    取代的胍衍生物，其制备方法及其药物用途

    公开(公告)号：US5977100A

    公开(公告)日：1999-11-02

    申请号：US074462

    申请日：1998-05-08

    申请人： Masahumi Kitano ,  Naohito Ohashi

    发明人： Masahumi Kitano ,  Naohito Ohashi

    IPC分类号： C07D471/06 ,  C07D487/06 ,  C07D498/06 ,  A61K31/55 ,  C07D223/14 ,  C07D487/00

    CPC分类号： C07D471/06 ,  C07D487/06

    摘要： A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y.sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO-- or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.7, for example, an unsubstituted alkyl group or a substituted alkyl group, or a pharmaceutically acceptable acid addition salt thereof, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton (Na.sup.+ /H.sup.+) exchange transport system, for example, hyperpiesia, arrhythmia, angina pectoris, hypercardia, diabetes, organopathies due to ischemia or ischemia re-perfusion, troubles due to cerebral ischemia, diseases caused by cell over-proliferations, and diseases caused by trouble with endothelial cells.

    摘要翻译： 由以下通式表示的取代的胍衍生物：其中R1，R2，R3和R4独立地是氢原子，未取代的烷基，取代的烷基，卤素原子等; 可以相同或不同的Y 1，Y 2，Y 3，Y 4，Y 5，Y 6和Y 7独立地是单键，-CH 2 - ， - O-，-CO-等， Y1至Y7能够一起代表-CH = CH-，Y 1至Y 7中的至少两个独立地为单键以外的基团; Z可以不存在，或者一个或多个Z可以独立地存在于与构成由Y1至Y7形成的环的任何碳原子键合的氢原子的取代基，例如未取代的烷基 基团或取代的烷基或其药学上可接受的酸加成盐可用作由加速钠/质子（Na + / H +）交换转运系统引起的疾病的治疗或预防剂，例如高血压，心律失常 ，心绞痛，超心，糖尿病，由于局部缺血或缺血再灌注引起的有机病变，由于脑缺血引起的麻烦，由细胞过度增殖引起的疾病，以及由内皮细胞引起的疾病引起的疾病。

    Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof
    8.
    发明授权
    Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof 失效
    取代的胍衍生物，其制备方法及其药物用途

    公开(公告)号：US5834454A

    公开(公告)日：1998-11-10

    申请号：US790024

    申请日：1997-01-28

    申请人： Masahumi Kitano ,  Naohito Ohashi

    发明人： Masahumi Kitano ,  Naohito Ohashi

    IPC分类号： C07D471/06 ,  C07D487/06 ,  C07D498/06 ,  A61K31/33 ,  C07D225/04 ,  C07D487/00 ,  C07D491/00

    CPC分类号： C07D471/06 ,  C07D487/06

    摘要： A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y .sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO--or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.7, for example, an unsubstituted alkyl group or a substituted alkyl group, or a pharmaceutically acceptable acid addition salt thereof, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton (Na.sup.+ /H.sup.+) exchange transport system, for example, hyperpiesia, arrhythmia, angina pectoris, hypercardia, diabetes, organopathies due to ischemia or ischemia re-perfusion, troubles due to cerebral ischemia, diseases caused by cell overproliferations, and diseases caused by trouble with endothelial cells.

    摘要翻译： 由以下通式表示的取代胍衍生物：其中R 1，R 2，R 3和R 4独立地为氢原子，未取代的烷基，取代的烷基，卤素原子等; 可以相同或不同的Y 1，Y 2，Y 3，Y 4，Y 5，Y 6和Y 7独立地是单键，-CH 2 - ， - O-，-CO-等， Y1至Y7可以一起代表-CH = CH-，Y1至Y7中的至少两个独立地为单键以外的基团; Z可以不存在，或者一个或多个Z可以独立地存在于与构成由Y1至Y7形成的环的任何碳原子键合的氢原子的取代基，例如未取代的烷基 基团或取代的烷基或其药学上可接受的酸加成盐可用作由加速钠/质子（Na + / H +）交换转运系统引起的疾病的治疗或预防剂，例如高血压，心律失常 ，心绞痛，超心，糖尿病，由于局部缺血或缺血再灌注引起的有机病变，由于脑缺血引起的麻烦，由细胞过度增殖引起的疾病，以及由内皮细胞引起的疾病引起的疾病。